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1. 发明专利

JP2014005206A Arylamino heterocyclic carboxamide compound 审中-公开
标题翻译： ARYLAMINO杂环碳酰胺化合物
公开(公告)号：JP2014005206A
公开(公告)日：2014-01-16
申请号：JP2010236958
申请日：2010-10-22
申请人： Astellas Pharma Inc , アステラス製薬株式会社 , Kotobuki Seiyaku Kk , 壽製薬株式会社
发明人： SHIMADA ITSURO , MATSUYA TAKAHIRO , KUROSAWA KAZUO , IIKUBO KAZUHIKO , KAMIKAWA AKIO , KUROMITSU SADAO , SHINTO NOBUAKI , FUTAMI TAKASHI , KAWASE TATSUYA , SANO YORIMASA , YAMANAKA AYA , NISHIMURA KOICHI , ASAUMI MAKOTO , TOMIYAMA YASUSHI , IWAI TATSUNORI
IPC分类号： C07D239/06 , A61K31/497 , A61K31/506 , A61K31/5377 , A61K31/541 , A61P11/00 , A61P35/00 , A61P43/00 , C07D241/20 , C07D401/14 , C07D403/12 , C07D405/14 , C07D409/14 , C07D413/14 , C07D451/02 , C07D471/10 , C07D487/04 , C07D487/08 , C07D491/20 , C07D493/08
CPC分类号： C07D493/08 , C07D239/06 , C07D241/20 , C07D401/14 , C07D403/12 , C07D405/14 , C07D409/14 , C07D413/14 , C07D451/02 , C07D471/10 , C07D487/04 , C07D487/08 , C07D491/20
摘要： PROBLEM TO BE SOLVED: To provide a compound useful as an inhibitor of a kinase activity of EML4-ALK fusion protein.SOLUTION: The present inventors conducted intensive studies about a compound having an inhibitory activity of the kinase activity of EML4-ALK fusion protein and found that the arylamino heterocyclic carboxamide compound of the present invention has the inhibitory activity of the kinase activity of EML4-ALK fusion protein, and completed the present invention. The compound of the present invention may be used for a pharmaceutical composition for preventing and/or treating cancer, lung cancer, non-small cell lung cancer, small cell lung cancer and the like.
摘要翻译：要解决的问题：提供可用作EML4-ALK融合蛋白的激酶活性抑制剂的化合物。解决方案：本发明人对具有EML4-ALK融合蛋白激酶活性抑制活性的化合物进行了深入研究，发现本发明的芳基氨基杂环羧酰胺化合物具有EML4-ALK融合蛋白的激酶活性的抑制活性，完成了本发明。本发明的化合物可以用于预防和/或治疗癌症，肺癌，非小细胞肺癌，小细胞肺癌等的药物组合物。

2. 发明专利

JP2013234194A Method of producing c-glycoside derivative 有权
标题翻译：生产C-谷氨酰胺衍生物的方法
公开(公告)号：JP2013234194A
公开(公告)日：2013-11-21
申请号：JP2013153374
申请日：2013-07-24
申请人： Kotobuki Seiyaku Kk , 壽製薬株式会社 , Astellas Pharma Inc , アステラス製薬株式会社
发明人： TOMIYAMA YASUSHI , YOKOTA MASAYUKI
IPC分类号： C07H15/04
CPC分类号： C07H15/04 , C07H1/00
摘要： PROBLEM TO BE SOLVED: To provide a technology of producing C-glycoside derivatives at high efficiency under industrially advantageous conditions.SOLUTION: C-glycoside derivatives can be produced in a short time and high yield while avoiding an ultra-low temperature reaction when utilizing a coupling reaction using aryl magnesate.
摘要翻译：要解决的问题：提供在工业上有利条件下以高效率生产C-糖苷衍生物的技术。解决方案：可以在短时间和高产量下生产C-糖苷衍生物，同时避免超低温反应使用芳基镁酸酯进行偶联反应。

3. 发明专利

JP2009046489A C-glycoside derivative or salt thereof 有权
标题翻译： C-GLYCOSIDE衍生物或其盐
公开(公告)号：JP2009046489A
公开(公告)日：2009-03-05
申请号：JP2008222927
申请日：2008-08-29
申请人： Astellas Pharma Inc , Kotobuki Seiyaku Kk , アステラス製薬株式会社 , 壽製薬株式会社
发明人： IMAMURA MASAKAZU , MURAKAMI TAKESHI , SHIRAKI RYOTA , IKUGAI KAZUHIRO , SUGANE TAKASHI , IWASAKI SHIRO , KUROSAKI HIDESHI , TOMIYAMA YASUSHI , NODA ATSUSHI , KITSUTA KAYOKO , KOBAYASHI YOSHINORI
IPC分类号： C07D309/10 , A61K31/351 , A61K31/381 , A61K31/4025 , A61K31/4035 , A61K31/404 , A61K31/41 , A61K31/4184 , A61K31/423 , A61K31/427 , A61K31/428 , A61K31/4433 , A61K31/497 , A61K31/5377 , A61P3/04 , A61P3/10 , A61P5/50 , A61P43/00 , C07D207/06 , C07D333/12 , C07D333/16 , C07D333/54 , C07D405/04 , C07D405/10 , C07D407/04 , C07D407/10 , C07D409/04 , C07D409/10 , C07D409/14 , C07D413/10 , C07D417/10 , C07D493/04 , C07D495/04
CPC分类号： C07D495/04 , A61K31/351 , A61K31/381 , A61K31/4035 , A61K31/404 , A61K31/41 , A61K31/4184 , A61K31/423 , A61K31/428 , A61K31/4433 , A61K31/497 , A61K31/5377 , C07D405/10 , C07D407/10 , C07D409/10 , C07D413/10 , C07D417/10
摘要： PROBLEM TO BE SOLVED: To provide a compound useful as an agent for treating various types of diabetes such as non-insulin-dependent diabetes (type II diabetes) and insulin-dependent diabetes (type I diabetes) and in addition, various diabetes-related diseases including insulin-resistant diseases and obesity. SOLUTION: This compound is a C-glycoside derivative having hetero rings each containing at least one heteroatom selected from N, S, and O as a substituent or is a salt thereof. COPYRIGHT: (C)2009,JPO&INPIT
摘要翻译：待解决的问题：提供可用作治疗各种类型的糖尿病如非胰岛素依赖性糖尿病（II型糖尿病）和胰岛素依赖型糖尿病（I型糖尿病）的药剂的化合物，另外还可以使用各种糖尿病相关疾病，包括胰岛素抵抗疾病和肥胖。解决方案：该化合物是具有各自含有至少一个选自N，S和O的杂原子作为取代基的杂环的C-糖苷衍生物或其盐。版权所有（C）2009，JPO＆INPIT

4. 发明专利

JP2008001596A Sodium channel inhibitor 审中-公开
标题翻译：钠通道抑制剂
公开(公告)号：JP2008001596A
公开(公告)日：2008-01-10
申请号：JP2004257280
申请日：2004-09-03
申请人： Astellas Pharma Inc , Kotobuki Seiyaku Kk , アステラス製薬株式会社 , 壽製薬株式会社
发明人： KIKUCHI KAZUMI , FUJIYASU JIRO , WATANABE TOSHIHIRO , NAGAKURA TOUKI , TOMIYAMA YASUSHI , SONEGAWA MOTOHARU , TOKUZAKI KAZUO , IWAI TATSUNORI
IPC分类号： C07D211/10 , A61K31/4465 , A61K31/4535 , A61P25/04 , C07D211/18 , C07D211/22 , C07D409/04
CPC分类号： C07D211/10 , C07D211/18 , C07D211/22 , C07D409/04
摘要： PROBLEM TO BE SOLVED: To obtain a sodium channel inhibitor having a high analgesic effect on neuropathic pain and a reduced adverse effect, a new piperidine derivative useful as a sodium channel inhibitor or its physiologically acceptable salt and a pharmaceutical composition containing the same as an active ingredient.
SOLUTION: The sodium channel inhibitor contains as an active ingredient a piperidine derivative or a pharmaceutically acceptable salt thereof. The derivative or salt has a structure in which the piperidine ring is directly bonded to a benzene ring or hetero ring and the benzene ring or hetero ring is directly bonded to another benzene ring.
COPYRIGHT: (C)2008,JPO&INPIT
摘要翻译：要解决的问题为了获得对神经性疼痛具有高镇痛作用和减少的副作用的钠通道抑制剂，可用作钠通道抑制剂或其生理学上可接受的盐的新的哌啶衍生物和含有它们的药物组合物作为活性成分。解决方案：钠通道抑制剂含有哌啶衍生物或其药学上可接受的盐作为活性成分。该衍生物或盐具有其中哌啶环直接键合到苯环或杂环的结构，苯环或杂环与另一苯环直接结合。版权所有（C）2008，JPO＆INPIT

5. 发明专利

JP2009062381A Glucolipid derivative, its manufacturing method and medicine containing it as effective component 有权
标题翻译：葡萄糖衍生物及其制造方法和药物作为有效成分
公开(公告)号：JP2009062381A
公开(公告)日：2009-03-26
申请号：JP2008263962
申请日：2008-10-10
申请人： Kotobuki Seiyaku Kk , 壽製薬株式会社
发明人： TOMIYAMA YASUSHI , YANAGISAWA TAKASHI , FUTAMURA MASAYUKI , NODA ATSUSHI , TOMIYAMA TAKESHI
IPC分类号： C07D309/10 , A61K31/351 , A61P35/00 , A61P35/04 , A61P37/04
摘要： PROBLEM TO BE SOLVED: To provide a glucolipid derivative having an α-S-glucosidic linkage which is useful as an antitumor medicine and an immunopotentiator, and its manufacturing method, and medicines containing it as an effective component. SOLUTION: This glucolipid derivative is a compound represented by general formula (I) (wherein W is a 9-17C saturated or unsaturated carbon chain and further in some case contains a hydroxy group, X is an 11-25C saturated or unsaturated carbon chain and further in some case contains a hydroxy group, Y represents -S(O) 0-2 CH 2 -, Z represents -CO- or -SO 2 -, R represents -CH 2 OH, -CO 2 H, -CO 2 OCH 2 CO 2 H, or -CH 2 OSO 3 H group, and R 0 represents -OH, -NH 2 , or -NHAc group), or its pharmaceutically permissible salts. COPYRIGHT: (C)2009,JPO&INPIT
摘要翻译：待解决的问题：提供可用作抗肿瘤药和免疫增强剂的具有α-S-糖苷键的糖脂衍生物及其制备方法以及含有它作为有效成分的药物。解决方案：该糖脂衍生物为通式（I）表示的化合物（其中W为9-17C饱和或不饱和碳链，并且在某些情况下还含有羟基，X为11-25℃饱和或不饱和的碳链，并且在某些情况下还含有羟基，Y表示-S（O），S表示-CO-或-SO 2 - ，R表示-CH 2 OH，-CO 2 H，-CO 2 / SB> CO 2 H或-CH 2 OSO 3 H基，R SB 0表示-OH ，-NH 2 SBA或-NHAc基团）或其药学上允许的盐。版权所有（C）2009，JPO＆INPIT

6. 发明专利

JP2006008549A Drug for treating or preventing double onset of hypertension and serum hyperuricemia and/or hypercholesterolemia 有权
标题翻译：用于治疗或预防高血压和血清胰岛素和/或胆固醇的双重作用的药物
公开(公告)号：JP2006008549A
公开(公告)日：2006-01-12
申请号：JP2004184906
申请日：2004-06-23
申请人： Kotobuki Seiyaku Kk , 壽製薬株式会社
发明人： TOMIYAMA ITARU , TOMIYAMA YASUSHI , MIYAMOTO HIDETOSHI , HAYASHI KEIICHIRO , MOCHIZUKI SEIICHIRO
IPC分类号： A61K31/357 , A61K31/549 , A61K45/00 , A61P3/06 , A61P7/10 , A61P9/12 , A61P19/06 , A61P43/00 , C07D257/04
CPC分类号： A61K31/4184
摘要： PROBLEM TO BE SOLVED: To provide a drug for preventing or treating an overlap of hypertension and hyperuricemia and/or hypercholesterolemia which are the risk-factors of adult disease. SOLUTION: The drug for treating or preventing hypertension and serum hyperuricemia and/or hypercholesterolemia has 2-propyl-3-ä[2'-(1H-tetrazol-5-yl)biphenyl-4-yl]methyl}-5,6,7,8-tetrahydrocycloheptaimidazol-4(3H)-one, its prodrug or its salt (generic name: pratosartan) as an active ingredient. The pratosartan may be combined with one or more diuretics selected from the group consisting of sulfonamide diuretics, phenoxyacetic acid diuretics, and thiazide diuretics. Further, the pratosarton may be combined with one or more hypolipidemic agents selected from statins, fibrates, cholesterol adsorbents, cholesterol absorption inhibitors, and cholesterol dissimilation excretion accelerators. COPYRIGHT: (C)2006,JPO&NCIPI
摘要翻译：要解决的问题：提供用于预防或治疗作为成人疾病的危险因素的高血压和高尿酸血症和/或高胆固醇血症重叠的药物。解决方案：用于治疗或预防高血压和血清高尿酸血症和/或高胆固醇血症的药物具有2-丙基-3-ä[2' - （1H-四唑-5-基）联苯-4-基]甲基} -5 ，6,7,8-四氢环庚胺咪唑-4（3H） - 酮，其前药或其盐（通用名：普拉沙沙坦）作为活性成分。普拉沙沙坦可以与选自磺酰胺利尿剂，苯氧基乙酸利尿剂和噻嗪类利尿剂的一种或多种利尿剂组合。此外，普拉托斯顿可以与选自他汀类，贝特类，胆固醇吸附剂，胆固醇吸收抑制剂和胆固醇异化排泄促进剂的一种或多种降血脂药合并。版权所有（C）2006，JPO＆NCIPI

7. 发明专利

JP2004137183A Oral administration medicine, health food product or nutritional medicine composition containing glucosaminoglycan or its salt 审中-公开
公开(公告)号：JP2004137183A
公开(公告)日：2004-05-13
申请号：JP2002302520
申请日：2002-10-17
申请人： Kotobuki Seiyaku Kk , 壽製薬株式会社
发明人： TOMIYAMA YASUSHI , TOIDA TOSHIHIKO
IPC分类号： A23L1/30 , A61K31/726 , A61K31/728 , A61K31/737 , A61K36/48 , A61P3/06 , A61P13/02 , A61P13/12 , A61P19/02 , A61K35/78
摘要： PROBLEM TO BE SOLVED: To obtain a medicine, a health food and a nutritional medicine composition each of which can improve the oral absorption of glucosaminoglycan or its salt, can enhance its original medicinal effects, and quickly exhibits the effects. SOLUTION: The oral administration medicine, health food or nutritional medicine composition is characterized by comprising one or more compounds selected from the group consisting of glucosaminoglycan or its salts and one or more compounds selected from the group consisting of saponin and its salts. The glucosaminoglycan or its salts include hyaluronic acid, hyaluronate, dermatan sulfuric acid, dermatan sulfate, chondroitin, chondroitin sulfuric acid, and chondroitin sulfate. The saponin is preferably soybean saponin. The mass ratio of one or more compounds selected from the group consisting of glucosaminoglycan and its salts: one or more compounds selected from the group consisting of saponin and its salts is preferably 1:0.0001 to 2. COPYRIGHT: (C)2004,JPO

8. 发明专利

JP2013010712A Tricyclic compound and pharmaceutical composition containing the same 有权
标题翻译：三元复合物和含有它们的药物组合物
公开(公告)号：JP2013010712A
公开(公告)日：2013-01-17
申请号：JP2011144216
申请日：2011-06-29
申请人： Kotobuki Seiyaku Kk , 壽製薬株式会社
发明人： TOMIYAMA TAKESHI , TOMIYAMA YASUSHI , YOKOTA MASAYUKI , MUROGA SHOTA
IPC分类号： C07D409/12 , A61K31/403 , A61K31/407 , A61K31/422 , A61K31/433 , A61K45/00 , A61P7/02 , A61P9/10 , A61P29/00 , A61P43/00 , C07D209/80 , C07D209/88 , C07D409/14 , C07D413/12 , C07D417/12 , C07D417/14 , C07D471/04 , C07D491/052 , C07D491/113 , C07D495/04
摘要： PROBLEM TO BE SOLVED: To provide a compound which provides EP3 receptor antagonism, and a pharmaceutical composition which contains the compound and is for prevention against and treatment of prostaglandin mediated disorders.SOLUTION: There is disclosed the compound represented by general formula (I), where Rand Rare a hydrogen atom, a lower alkyl group, a lower haloalkyl group, a lower alkoxy group, or a halogen atom, Ris a monocyclic or bicyclic aromatic ring or heterocyclic ring, or a cyclo ring, Ris a monocyclic or bicyclic aromatic ring or heterocyclic ring, X is -CH- or a carbon atom having a lower alkyl group, Y is -CHCH-(CH)m- or -CR=CR-(CH)m- (Rand Rmay be identical or different and a hydrogen atom or a halogen atom), -O-CH-(CH)m-, (cyclo ring (1-5 carbons))-(CH)m-, or (monocyclic or bicyclic aromatic ring)-(CH)m-, where m is 0-5, Z is a bond or -SO-, and n is 0-5.
摘要翻译：待解决的问题：提供提供EP3受体拮抗作用的化合物和含有该化合物并用于预防和治疗前列腺素介导的病症的药物组合物。解决方案：公开了由通式（I）表示的化合物，其中R 1 和R 2 是氢原子，低级烷基，低级卤代烷基，低级烷氧基或卤素原子，单环或双环芳环或杂环，或环，R 4是单环或双环芳环或杂环，X是-CH 2，或碳原子具有低级烷基，Y是-CH 2 - （CH 2 < / SB>）m-或-CR 5 = CR 6 - （CH 2 < / SB>）m-（R 5 和R 6 可以相同或不同，氢原子或卤素原子），-O-CH 2 - （CH 2 ）m-，（环环（1-5个碳）） - （ m - 或（单环或双环芳环） - （CH 2 ）m-，其中m为0 -5，Z是一个债券o r -SO 2 - ，n为0-5。版权所有（C）2013，JPO＆INPIT

9. 发明专利

JP2008031131A Method for producing oxazolidine derivative 有权
标题翻译：生产氧杂环丁烷衍生物的方法
公开(公告)号：JP2008031131A
公开(公告)日：2008-02-14
申请号：JP2006209419
申请日：2006-08-01
申请人： Kotobuki Seiyaku Kk , 壽製薬株式会社
发明人： TOMIYAMA YASUSHI , YOKOTA MASAYUKI
IPC分类号： C07D263/26
CPC分类号： Y02P20/55
摘要： PROBLEM TO BE SOLVED: To provide a method for producing a compound represented by formula (VI) in a high yield at a low cost. SOLUTION: This method for producing a compound represented by formula (VI) comprises the first process for protecting the hydroxyl group of a compound of formula (I) (R 1 is a lower alkyl, allyl, phenyl, or benzyl) with a tetrahydropyranyl group or a substituent-having silyl group, the second process for hydrolyzing the ester to obtain a compound of formula (III) (R 2 is the tetrahydropyranyl or the substituent-having silyl), the third process for converting the compound into a mixed acid anhydride and then reacting with optically active 4-phenyl-2-oxazolidinone, and the fourth process for removing the protecting group from the obtained compound. COPYRIGHT: (C)2008,JPO&INPIT
摘要翻译：待解决的问题：提供以低成本高产率制备由式（VI）表示的化合物的方法。解决方案：用于制备由式（VI）表示的化合物的方法包括保护式（I）化合物的羟基的第一种方法（R 1 SP 1是低级烷基，烯丙基，苯基或苄基）与四氢吡喃基或具有取代基的甲硅烷基取代，第二种水解酯的方法得到式（III）化合物（R 2 SP 2）是四氢吡喃基或取代基 - 甲硅烷基），第三种将化合物转化为混合酸酐然后与光学活性4-苯基-2-恶唑烷酮反应的方法，以及从所得化合物中除去保护基团的第四种方法。版权所有（C）2008，JPO＆INPIT

10. 发明专利

JP2006298791A Medicine for oral administration, health food or nutrient chemical composition containing glycosaminoglycan or its salt 审中-公开
标题翻译：用于口服药物，含有谷氨酰胺糖胺或其盐的健康食品或营养化学成分的药物
公开(公告)号：JP2006298791A
公开(公告)日：2006-11-02
申请号：JP2005119753
申请日：2005-04-18
申请人： Kotobuki Seiyaku Kk , 壽製薬株式会社
发明人： TOMIYAMA YASUSHI
IPC分类号： A61K31/726 , A23L1/30 , A61K31/728 , A61K31/737 , A61K47/26 , A61P17/00 , A61P19/04 , A61P27/10
摘要： PROBLEM TO BE SOLVED: To provide a medicine, health food, nutrient medical composition and external preparation having improved peroral absorption of glycosaminoglycan or its salt, increased original drug action of the component and quick action. SOLUTION: The medicine for oral administration, health food and nutrient medical composition contain glycosaminoglycan or its salt and glycyrrhizinic acid or its salt. Examples of the glycosaminoglycan or its salt are hyaluronic acid, hyaluronate, dermatan sulfuric acid, dermatan sulfate, chondroitin, chondroitin sulfuric acid, and chondroitin sulfate. The agent may further contain saponin or its salt. The compounding mass ratio of glycyrrhizinic acid or its salt to glycosaminoglycan or its salt is preferably 1:(0.0001-2). COPYRIGHT: (C)2007,JPO&INPIT
摘要翻译：要解决的问题：提供具有改善的糖胺聚糖或其盐的口服吸收的药物，保健食品，营养物质组合物和外用制剂，增加了组分的原始药物作用和快速作用。
解决方案：口服药物，保健食品和营养成分含有糖胺聚糖或其盐和甘草酸或其盐。糖胺聚糖或其盐的实例是透明质酸，透明质酸盐，皮肤素硫酸，硫酸皮肤素，软骨素，硫酸软骨素和硫酸软骨素。该试剂还可以含有皂苷或其盐。甘草酸或其盐与糖胺聚糖或其盐的配合质量比优选为1：（0.0001-2）。版权所有（C）2007，JPO＆INPIT

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